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Database of Antiretroviral Drug Interactions

Interactions with Rifabutin and Antiretrovirals

Antiretroviral (ARV)Dose of ARVDose of RifabutinEffect on ARV LevelsEffect on Rifabutin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Amprenavir340
(APV)(Agenerase)
1200 mg BID300 mg QD x 14 daysNo significant changeRifabutin AUC: increased 193%; Cmax: increased 119%; 25-O-desacetylrifabutin AUC: increased 1230%; clearance: decreased 66%Increased rifabutin effects (eg, uveitis)Inhibition of CYP450 3A4 by amprenavir

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Amprenavir60, 62, 63
(APV)(Agenerase)
1200 mg BID x 10 days300 mg QD x 10 daysAmprenavir AUC: decreased 15%; Cmax: no significant change; Cmin: decreased 15%Rifabutin AUC: increased 193%; Cmax: increased 119%; Cmin: increased 271%Increased rifabutin effects (eg, uveitis)Inhibition of CYP450 3A4 by amprenavir

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Atazanavir341
(ATV)(Reyataz)
400 mg QD on days 1-14, 400 mg QD with ritonavir 100 mg QD on days 15-28150 mg QD on days 15-28Atazanavir AUC: increased 191%; Cmax: increased 81%Not studiedIncreased atazanavir effects-

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Atazanavir341
(ATV)(Reyataz)
400 mg QD on days 1-28150 mg QD on days 15-28Atazanavir Cmax: increased 34%Not studied--

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Atazanavir
(ATV)(Reyataz)
600 mg QD on days 11-20300 mg QD on days 1-10, then 150 mg QD on days 11-20Not studiedRifabutin AUC: increased 110%; Cmax: increased 118%; Cmin: increased 243%; 25-O-desacetylrifabutin AUC: increased 2101%; Cmax: increased 720%; Cmin: increased 7460%Increased rifabutin effects (eg, uveitis)Inhibition of CYP450 3A4 by atazanavir

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Antiretroviral (ARV)Dose of ARVDose of RifabutinEffect on ARV LevelsEffect on Rifabutin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Atazanavir/cobicistat755, 727
(others)(Evotaz)
---Not studied; may increase rifabutin levels--

Use rifabutin 150 mg once daily or 300 mg three times a week. Monitor for antimycobacterial activity and consider therapeutic drug monitoring.

Bictegravir759
(Biktarvy)
75 mg daily300 mg daily (fasted)Cmax decreased 20%; AUC decreased 38%; Cmin decreased 56%Not studiedPotentially loss of antiviral efficacy-

Use alternative agents

Darunavir417
(DRV)(Prezista)
600 mg Q12H150 mg QODDarunavir AUC: increased 57%; Cmin: increased 75%; Cmax: increased 42% Ritonavir AUC: increased 66%; Cmin: increased 31%; Cmax: increased 68%Rifabutin AUC: no significant change; Cmin: increased 64%; Cmax: decreased 28% 25-O-desacetylrifabutin AUC: increased 881%; Cmin: increased 2610%; Cmax: increased 377%Increased darunavir and rifabutin effects. Note thatlLower rifabutin exposure has been reported in HIV- infected patients as compared to healthy study participants.Inhibition of CYP450 3A4 by darunavir

Use rifabutin 150 mg once daily or 300 mg three times a week. Monitor for antimycobacterial activity and consider therapeutic drug monitoring.

Darunavir/cobicistat727
(Prezcobix)
--- Not studied; may increase rifabutin levels--

Use rifabutin 150 mg once daily or 300 mg three times a week. Monitor for antimycobacterial activity and consider therapeutic drug monitoring.

Delavirdine88
(DLV)(Rescriptor)
400 mg TID300 mg QDDelavirdine AUC: decreased 80%Rifabutin AUC: increased 100%Decreased delavirdine effects; increased rifabutin effects (eg, uveitis)Induction of CYP450 3A4 by rifabutin; inhibition of CYP450 3A4 by delavirdine

Do not coadminister

Didanosine84
(ddI)(Videx)
167 mg or 250 mg (buffered formulation) Q12H x 12 days300 mg or 600 mg QD x 12 daysDidanosine AUC: no significant change; Cmax: increased 17%Not studied--

No dose adjustment necessary

Antiretroviral (ARV)Dose of ARVDose of RifabutinEffect on ARV LevelsEffect on Rifabutin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Dolutegravir641
(Tivicay)
50 mg QD300 mg QDDolutegravir Cmin: decreased 30% ---

No dose adjustment necessary

Efavirenz338
(EFV)(Sustiva)
600 mg QD600 mg twice weeklyNot studiedRifabutin AUC: no significant change; Cmax: no significant change (when compared to rifabutin 300 mg twice weekly without efavirenz)--

No dose adjustment necessary

Efavirenz
(EFV)(Sustiva)
600 mg QD300 mg or 450 mg twice weeklyNot studiedOn 300 mg rifabutin twice weekly, rifabutin level 2 hours after dose: no significant change; rifabutin level 6 hours post dose: decreased 27%; on 450 mg twice weekly, rifabutin level 2 hours post dose: no significant change; rifabutin level 6 hours post dose: decreased 58%(all values compared to rifabutin alone)Possibly decreased rifabutin effectsInduction of CYP450 3A4 by efavirenz

Increase rifabutin to 450-600 mg QD

Efavirenz90, 345
(EFV)(Sustiva)
600 mg x 14 days300 mg QD x 14 daysNo significant changeRifabutin AUC: decreased 38%; Cmax: decreased 32%Decreased rifabutin effectsInduction of CYP450 3A4 by efavirenz

Increase rifabutin to 450-600 mg QD

Elvitegravir697
(Vitekta)
300 mg plus 100 mg ritonavir150 mg every other dayNo effectIncreased rifabutin levels and increased rifabutin metabolite (25-O-desacetylrifabutin). Potential increase of 25-O-desacetylrifabutin AUC of 951% if given with elvitegravir with a ritonavir-boosted protease inhibitorPotential for increased rifabutin toxicityInhibition of CYP3A4

Use rifabutin 150mg once daily or 300 mg three times weekly if co-administering with elvitegravir and a ritonavir-boosted PI. Monitor for antimycobacterial activity and consider therapeutic drug monitoring.

Elvitegravir/cobicistat639, 623
(Genvoya, Stribild)
150 mg/150 mg150 mg every other dayElvitegravir AUC: decreased 21%; Cmin: decreased 67%25-O-rifabutin AUC: increased 625%; Cmin: increased 494% (compared to 300 mg rifabutin alone)Increased rifabutin effects-

Do not coadminister; consider alternative antiretrovirals.

Antiretroviral (ARV)Dose of ARVDose of RifabutinEffect on ARV LevelsEffect on Rifabutin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Elvitegravir/ritonavir-boosted protease inhibitor697
---Increased AUC of 25-O-desacetyl-rifabutin (metabolite) by 951%Increased rifabutin adverse effects (e.g. uveitis)Inhibition of CYP450 3A4 by ritonavir

Use rifabutin 150mg once daily or 300 mg three times weekly if co-administering with elvitegravir and a ritonavir-boosted PI. Monitor for antimycobacterial activity and consider therapeutic drug monitoring.

Etravirine405
(ETR)(Intelence)
-300 mg QDEtravirine AUC: decreased 37%; Cmax: decreased 37%; Cmin: decreased 35%Rifabutin AUC: decreased 17%; Cmin: decreased 24%; 25-O-desacetylrifabutin AUC: decreased 17%; Cmax: decreased 15%; Cmin: decreased 22%Decreased rifabutin effectsInduction of CYP450 by etravirine

If administered with etravirine and NO protease inhibitor, rifabutin coadministration is acceptable. If etravirine and a protease inhibitor are used together, consider alternate agents to rifabutin if at all possible.

Fosamprenavir420
(FPV)(Lexiva)
700 mg BID with 100 mg ritonavir BID150 mg QODAmprenavir AUC: increased 35%; Cmax: increased 36%;, Cmin: increased 17% (compared to historical controls)Rifabutin: no significant change; Desacetylrifabutin AUC: increased 1010%; Cmin: increased 1020%; Cmax: increased 479%; Rifabutin and metabolite AUC: increased 64% (compared to rifabutin 300 mg QD when given alone)-Inhibition of CYP450 3A4 by fosamprenavir/ritonavir

Dose adjust rifabutin 150 mg once daily or 300 mg three times a week.

Indinavir343
(IDV)(Crixivan)
1000 mg Q8H150 mg QD x 14 daysIndinavir AUC: increased 15%Rifabutin AUC: increased 60% (when compared to rifabutin 300 mg QD monotherapy); 25-desacetyl rifabutin AUC: increased 125% (when compared to 25-desacetyl rifabutin from rifabutin 300 mg QD monotherapy)Increased rifabutin effects (eg, uveitis)Induction of CYP450 3A4 by rifabutin

Decrease rifabutin to 150 mg QD or 300 mg 3 times/week and increase indinavir to 1000 mg Q8H

Indinavir342, 16, 254
(IDV)(Crixivan)
800 mg Q8H300 mg QDIndinavir AUC: decreased 32%Rifabutin AUC: increased 204%Increased rifabutin effects (eg, uveitis); decreased indinavir effectsInhibition of CYP450 3A4 by indinavir; induction of CYP450 3A4 by rifabutin

Decrease rifabutin to 150 mg QD or 300 mg 3 times/week and increase indinavir to 1000 mg Q8H

Indinavir342, 16, 254
(IDV)(Crixivan)
800 mg Q8H x 1 week150 mg QDIndinavir AUC: decreased 31%; AUC of indinavir 800 mg Q8H is comparable to that of 1000 mg Q8H if given with rifabutinRifabutin AUC: increased 60%Increased rifabutin effects (eg, uveitis); decreased indinavir effectsInhibition of CYP450 3A4 by indinavir; induction of CYP450 3A4 by rifabutin

Decrease rifabutin to 150 mg QD or 300 mg 3 times/week and increase indinavir to 1000 mg Q8H

Antiretroviral (ARV)Dose of ARVDose of RifabutinEffect on ARV LevelsEffect on Rifabutin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Indinavir337
(IDV)(Crixivan)
800 mg Q8H x 10 days150 mg QD x 10 daysIndinavir AUC: decreased 32%Rifabutin AUC: increased 54% (compared to 300 mg rifabutin)Increased rifabutin effects (eg, uveitis); decreased indinavir effectsInhibition of CYP450 3A4 by indinavir

Decrease rifabutin to 150 mg QD or 300 mg 3 times/week and increase indinavir to 1000 mg Q8H

Indinavir337
(IDV)(Crixivan)
800 mg Q8H x 10 days300 mg QD x 10 daysIndinavir AUC: decreased 34%Rifabutin AUC: increased 173%Increased rifabutin effects (eg, uveitis); decreased indinavir effectsInhibition of CYP450 3A4 by indinavir

Decrease rifabutin to 150 mg QD or 300 mg 3 times/week and increase indinavir to 1000 mg Q8H

Lopinavir/ritonavir737
(LPV/r)(Kaletra)
400 mg with 100 mg ritonavir x 14 days300 mg daily x 2-4 weeks, then 150 mg every other day x 2 weeks, then 300 mg every other dayNot studiedAUC for Rifabutin 150 mg every other day increased 10% when compared with rifabutin 300 mg daily . AUC for rifabutin 300 mg every other day increased 60% compared to 300 mg daily rifabutin.Potential toxicity from elevated rifabutin levels.-

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Lopinavir/ritonavir78
(LPV/r)(Kaletra)
400 mg/100 mg BID x 10 days300 mg QD x 10 days, 150 mg QD x 10 days-Rifabutin AUC: increased 203%; Cmax: increased 112%; Cmin: increased 390%; 25-O-desacetyl rifabutin AUC: increased 4650%; Cmax: increased 2260%; Cmin: increased 9390%Increased rifabutin effects (eg, uveitis)Inhibition of CYP450 3A4 by lopinavir/ritonavir

Use rifabutin dose of 150 mg daily or 300 mg 3times/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Lopinavir/ritonavir78
(LPV/r)(Kaletra)
400 mg/100 mg BID x 20 days150 mg QD x 10 daysLopinavir AUC: increased 17%; Cmax: no significant change; Cmin: increased 20%-Increased lopinavir/ritonavir effects-

Use rifabutin dose of 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Nelfinavir24
(NFV)(Viracept)
1250 mg Q12H x 7-8 days150 mg QD x 8 daysNo significant change---

Decrease rifabutin to 150 mg QD or 300 mg 2 to 3 times/week and increase nelfinavir to 1000 mg TID

Antiretroviral (ARV)Dose of ARVDose of RifabutinEffect on ARV LevelsEffect on Rifabutin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Nelfinavir345, 24
(NFV)(Viracept)
750 mg Q8H x 7-8 days150 mg QD x 8 daysNelfinavir AUC: decreased 23%; Cmax: decreased 18%Rifabutin AUC: increased 83%; Cmax: increased 19%Increased rifabutin effects (eg, uveitis); decreased nelfinavir effectsInhibition of CYP450 3A4 by nelfinavir; induction of CYP450 3A4 by rifabutin

Decrease rifabutin to 150 mg QD or 300 mg 2 to 3 times/week and increase nelfinavir to 1000 mg TID

Nelfinavir345, 24
(NFV)(Viracept)
750 mg Q8H x 7-8 days300 mg QD x 8 daysNelfinavir AUC: decreased 32%; Cmax: decreased 25%Rifabutin AUC: increased 207%; Cmax: increased 146%Increased rifabutin effects (eg, uveitis); decreased nelfinavir effectsInhibition of CYP450 3A4 by nelfinavir; induction of CYP450 3A4 by rifabutin

Decrease rifabutin to 150 mg QD or 300 mg 2 to 3 times/week and increase nelfinavir to 1000 mg TID

Nevirapine95
(NVP)(Viramune)
200 mg daily x 14 days; 200 mg150 mg vs 300 mg dailyNevirapine Cmin: decreased 16%AUC increased 17% and 25-O-desacetyl-rifabutin AUC increased 24%Decreased antiviral efficacyInduction of CYP450 3A4 by rifabutin

No dose adjustment necessary

Raltegravir432
(RAL)(Isentress)
400 mg BID300 mg QD x 14 dRaltegravir AUC: increased 19%; Cmax: increased 39%; Cmin: decreased 20%- - -

No dose adjustment necessary

Rilpivirine567
(RPV)(Edurant)
150 mg QD300 mg QDRilpivirine AUC: decreased 46%; Cmin: decreased 49%; Cmax: decreased 35%-Decreased rilpivirine effects-

Do not coadminister

Ritonavir344, 55
(RTV)(Norvir)
300 mg on day 15; 400 mg on day 16; 500 mg on days 17-24150 mg QD x 24 days-Rifabutin AUC: increased 400%; Cmax: increased 250%Increased rifabutin effects (eg, uveitis)Inhibition of CYP450 3A4 by ritonavir

Decrease rifabutin to 150 mg QOD or 300 mg 3 times/week

Antiretroviral (ARV)Dose of ARVDose of RifabutinEffect on ARV LevelsEffect on Rifabutin LevelsPotential Clinical EffectsMechanism of InteractionManagement
Saquinavir75
(SQV)(Fortovase, Invirase)
1200 mg TID300 mg x 1Saquinavir AUC: decreased 47%; Cmax: decreased 39%Rifabutin AUC: increased 44%; Cmax: increased 45%Increased rifabutin effectsinhibition of CYP450 3A4 by saquinavir

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Saquinavir339
(SQV)(Fortovase, Invirase)
400 mg with ritonavir 400 mg BID150 mg Q3D or 300 mg Q7D-Rifabutin weekly AUC: no significant difference between dosing regimensAvoidance of increased rifabutin effectsInhibition of CYP450 3A4 by both ritonavir and saquinavir

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Saquinavir44
(SQV)(Fortovase, Invirase)
600 mg (hard gel caps) TID x 14 days300 mg QD x 14 daysAUC: decreased 43%; Cmax: decreased 30%-Decreased saquinavir effectsInduction of CYP450 3A4 by rifabutin

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Stavudine275
(d4T)(Zerit)
40 mg BID300 mg QDStavudine AUC: no significant change; Cmax: decreased 30%; Cmin: increased 105%---

No dose adjustment necessary

Tipranavir154
(TPV)(Aptivus)
500 mg BID with 200 mg ritonavir BID x 15 doses150 mg x 1 doseNo significant changeRifabutin AUC: increased 190%; Cmax: increased 70%; Cmin: increased 114%; 25-O-desacetyl-rifabutin AUC: increased 1971%; Cmax: increased 220%; Cmin: increased 683%Increased rifabutin effects (eg, uveitis)Inhibition of CYP450 3A4 by tripranavir/ritonavir

Reduce rifabutin dose to 150 mg daily or 300 mg 3x/week. Monitor for antimicrobial activity and/or consider therapeutic drug monitoring.

Zidovudine81
(AZT, ZDV)(Retrovir)
-300 mg QD x 7 or 14 daysZidovudine half-life: decreased 28%---

No dose adjustment necessary

"-" indicates that there are no data available
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